HRP20040829A2 - Formulations of atorvastatin stabilized with alkali metal additions - Google Patents

Formulations of atorvastatin stabilized with alkali metal additions

Info

Publication number
HRP20040829A2
HRP20040829A2 HR20040829A HRP20040829A HRP20040829A2 HR P20040829 A2 HRP20040829 A2 HR P20040829A2 HR 20040829 A HR20040829 A HR 20040829A HR P20040829 A HRP20040829 A HR P20040829A HR P20040829 A2 HRP20040829 A2 HR P20040829A2
Authority
HR
Croatia
Prior art keywords
atorvastatin
sodium
alkali metal
formulations
carbonate
Prior art date
Application number
HR20040829A
Other languages
Croatian (hr)
Inventor
Bharat Singh Romi
Manoj Kumar Pananchukunnath
Malik Rajiv
Original Assignee
Ranbaxy Laboratories Limited
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Ranbaxy Laboratories Limited filed Critical Ranbaxy Laboratories Limited
Publication of HRP20040829A2 publication Critical patent/HRP20040829A2/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/401Proline; Derivatives thereof, e.g. captopril
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2009Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Inorganic Chemistry (AREA)
  • Obesity (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Farmaceutska formulacija koja poboljšava biološkudostupnost i biološku ujednačenost, podrazumijevačestice amorfnog i/ili kristaličnog atorvastatina, čija veličina (d90) ne prelazi 150 µm, a prosječna veličina čestica (d50) varira unutar raspona od5-50 µm. Atorvastatin može biti kalcij atorvastatin, magnezij atorvastatin, aluminij atorvastatin, željezo atorvastatin, cink atorvastatin, ili njihova kombinacija. Formulacije atorvastatina mogu se stabilizirati miješanjem atorvastatina s aditivom soli alkalnog metala koji je u ukupnoj težini formulacije zastupljen s 1.2% do manje od 5%. Aditiv soli alkalnog metala može biti natrijev karbonat, natrijev bikarbonat, natrijev hidroksid, natrijev silikat, dinatrij hidrogen ortofosfat, natrijev dihidrogen fosfat, dinatrijev hidrogen fosfat, natrijev fosfat, natrijev aluminat, kalcijev karbonat, kalcijev hidroksid, magnezijev karbonat, magnezijevhidroksid, magnezijev silikat, magnezijev aluminat, aluminij magnezijev hidroksid, odnosno jedna odnjihovih kombinacija. Formulacije atorvastatina koriste se u liječenju bolesti kao što je primarna hiperkolesterolemija, disbetalipoproteinemija te homozigotična familijama hiperkolesterolemija.A pharmaceutical formulation that improves bioavailability and biological uniformity comprises amorphous and / or crystalline atorvastatin particles, whose size (d90) does not exceed 150 µm, and the average particle size (d50) varies within the range of 5-50 (m. Atorvastatin may be atorvastatin calcium, atorvastatin magnesium, atorvastatin aluminum, atorvastatin iron, atorvastatin zinc, or a combination thereof. Atorvastatin formulations can be stabilized by mixing atorvastatin with an alkali metal salt additive which is present in the total weight of the formulation from 1.2% to less than 5%. The alkali metal salt additive may be sodium carbonate, sodium bicarbonate, sodium hydroxide, sodium silicate, disodium hydrogen orthophosphate, sodium dihydrogen phosphate, disodium hydrogen phosphate, sodium phosphate, sodium aluminate, calcium carbonate, carbonate, calcium carbonate, calcium magnesium aluminate, aluminum magnesium hydroxide, or one of their combinations. Atorvastatin formulations are used in the treatment of diseases such as primary hypercholesterolemia, dysbetalipoproteinemia, and homozygous families of hypercholesterolemia.

HR20040829A 2002-02-14 2004-09-13 Formulations of atorvastatin stabilized with alkali metal additions HRP20040829A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN112DE2002 2002-02-14
PCT/IB2003/000505 WO2003068191A1 (en) 2002-02-14 2003-02-14 Formulations of atorvastatin stabilized with alkali metal additions

Publications (1)

Publication Number Publication Date
HRP20040829A2 true HRP20040829A2 (en) 2006-07-31

Family

ID=27620520

Family Applications (1)

Application Number Title Priority Date Filing Date
HR20040829A HRP20040829A2 (en) 2002-02-14 2004-09-13 Formulations of atorvastatin stabilized with alkali metal additions

Country Status (23)

Country Link
US (1) US20030175338A1 (en)
EP (1) EP1336405A1 (en)
JP (1) JP2005522444A (en)
KR (1) KR20040101229A (en)
CN (1) CN1642526A (en)
AP (1) AP2004003112A0 (en)
AR (1) AR038839A1 (en)
AU (1) AU2003245736A1 (en)
BR (1) BR0307720A (en)
CA (1) CA2475722A1 (en)
CO (1) CO5600997A2 (en)
EA (1) EA200401059A1 (en)
EC (1) ECSP045235A (en)
HR (1) HRP20040829A2 (en)
IL (1) IL163550A0 (en)
IS (1) IS7404A (en)
MX (1) MXPA04007905A (en)
NO (1) NO20043790L (en)
OA (1) OA12777A (en)
PE (1) PE20030935A1 (en)
PL (1) PL371337A1 (en)
WO (1) WO2003068191A1 (en)
ZA (1) ZA200406970B (en)

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Also Published As

Publication number Publication date
IS7404A (en) 2004-08-13
ZA200406970B (en) 2005-06-20
IL163550A0 (en) 2005-12-18
PL371337A1 (en) 2005-06-13
CA2475722A1 (en) 2003-08-21
OA12777A (en) 2006-07-06
EP1336405A1 (en) 2003-08-20
NO20043790L (en) 2004-11-08
PE20030935A1 (en) 2003-10-30
AP2004003112A0 (en) 2004-09-30
ECSP045235A (en) 2004-09-28
US20030175338A1 (en) 2003-09-18
WO2003068191A1 (en) 2003-08-21
CO5600997A2 (en) 2006-01-31
EA200401059A1 (en) 2005-02-24
AR038839A1 (en) 2005-01-26
BR0307720A (en) 2005-01-25
AU2003245736A1 (en) 2003-09-04
MXPA04007905A (en) 2004-11-26
JP2005522444A (en) 2005-07-28
KR20040101229A (en) 2004-12-02
CN1642526A (en) 2005-07-20

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